SB-366791 has been used as a transient receptor potential cation channel subfamily V member 1 (TRPV1) antagonist:
to infer the in vitro and in vivo pharmacology of (E)-3-(4-t-butylphenyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acrylamide (AMG 9810)[1]
to study its effects on sodium hydrogen sulfide (NaHS) or capsaicin-induced contractile activity[2]
to study the inhibitory potency of phoneutria toxin (PnTx3-5) (native and recombinant) on various responses mediated by transient receptor potential cation channel subfamily V member 1 (TRPV1)[3]
Biochem/physiol Actions
SB-366791 might exhibit analgesic properties on bone cancer-related pain behavior.[4]
Vanilloid receptor-1 (TRPV1) antagonist.
Features and Benefits
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
The Journal of pharmacology and experimental therapeutics, 313(1), 474-484 (2004-12-24)
The vanilloid receptor 1 (VR1 or TRPV1) is a membrane-bound, nonselective cation channel expressed by peripheral sensory neurons. TRPV1 antagonists produce antihyperalgesic effects in animal models of inflammatory and neuropathic pain. Here, we describe the in vitro and in vivo
Dry eye disease (DED) is a highly prevalent ocular surface disorder with neuroimmune pathophysiology. Tear hyperosmolarity (THO), a frequent finding in affected patients, is considered a key element in DED pathogenesis, yet existing animal models are based on subjecting the
Capsaicin, an agonist of TRPV1, evokes intracellular [Ca2+] transients and glutamate release from perfused trigeminal ganglion. The spider toxin PnTx3-5, native or recombinant is more potent than the selective TRPV1 blocker SB-366791 with IC50 of 47 ± 0.18 nM, 45 ± 1.18 nM and 390 ± 5.1 nM in
Pharmacological investigation of hydrogen sulfide (H2S) contractile activity in rat detrusor muscle
Patacchini R, et al.
European Journal of Pharmacology, 509(2-3), 171-177 (2005)
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